二氢叶酸还原酶的体内测量及其被抗叶酸剂的抑制作用
In vivo measurement of dihydrofolate reductase and its inhibition by antifolates.
作者信息
Bowers S W, Duch D S
机构信息
Department of Medicinal Biochemistry, Wellcome Research Laboratories, Research Triangle Park, North Carolina 27709.
出版信息
Anal Biochem. 1988 Jul;172(1):169-75. doi: 10.1016/0003-2697(88)90427-7.
The ability of the enzyme dihydrofolate reductase to catalyze the formation of tetrahydrobiopterin from dihydrobiopterin was used to develop a method for measuring the activity of this enzyme in vivo. This method can be used to determine the activity of the enzyme in tissues as well as the extent and duration of inhibition of the enzyme by antifolates. Sepiapterin, which is converted to dihydrobiopterin by the enzyme sepiapterin reductase, was as effective a precursor as dihydrobiopterin and has been used in these studies because of its greater stability relative to dihydrobiopterin. Assay conditions must be established for each tissue and enzyme activity can be determined either by measuring the rate of disappearance of dihydrobiopterin or the rate of formation of tetrahydrobiopterin.
利用二氢叶酸还原酶催化二氢生物蝶呤形成四氢生物蝶呤的能力，开发了一种在体内测量该酶活性的方法。该方法可用于测定组织中酶的活性，以及抗叶酸剂对该酶的抑制程度和持续时间。由蝶呤还原酶转化为二氢生物蝶呤的蝶酰三谷氨酸，作为前体与二氢生物蝶呤一样有效，并且由于其相对于二氢生物蝶呤具有更高的稳定性，已用于这些研究中。必须为每个组织建立测定条件，并且可以通过测量二氢生物蝶呤的消失速率或四氢生物蝶呤的形成速率来确定酶活性。
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